DOI hydrochloride is a brain-permeable agonist of 5-HT_2A and 5-HT_2C receptors, with Ki values being 0.7, 2.4 and 20 nM for 5-HT_2A, 5-HT_2C and 5-HT_2B receptors, respectively. The 5-HT₂ receptor consists of three distinct subpopulations, i.e. 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors, among which the 5-HT_2A receptor contributes to the major part of the behavioral effects evoked by hallucinogens. DOI, as a phenylisopropylamine hallucinogen, can thus be used to explore 5-HT₂ receptor mediated biological events due to its high affinity for the 5-HT₂ receptor. In addition, DOI has also been used as an analytical reference standard categorized as a phenethylamine and amphetamine.

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